ArrestinDb

Finalizing display...

Ligand source activities (1 row/activity)

Affinity
Potency

Search:

	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

[D-Trp⁸]γ-MSH	1501	None	4	Human	Binding	IC50	=	1000.00	6.00	-	4	Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.7b01295
[D-Trp⁸]γ-MSH	1501	None	4	Human	Binding	IC50	=	1000.00	6.00	-	4	Inhibition of [125I]NDP-MSH binding to Melanocortin 1 receptor expressed in HEK293 cells; (N = 4)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049579s
[D-Trp⁸]γ-MSH	1501	None	4	Human	Binding	IC50	=	1.20	8.92	-	4	Inhibition of [125I]NDP-MSH binding to Melanocortin 1 receptor expressed in HEK293 cells; (N = 4)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049579s
ACTH	277	None	0	Human	Binding	pKi	=	-	8.60	2	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/7774675
ACTH	277	None	0	Human	Binding	pKi	=	8.60	8.07	2	5	None	Drug Central	-	-	-	-	-	-	-
ACTH-(4-10)	218797	125I-NDP-MSH	0	Human	Binding	pKi	=	106.00	6.97	7	4	-	PDSP KiDatabase	961.4	29	13	12	-1.46	CSCCC(N)C(=O)NC(CCC(=O)O)C(=O)NC(Cc1cnc[nH]1)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCC(=O)O	-
ACTH-(4-10)	218797	125I-[Nle4,D-Phe7]Alpha-MSH	0	Human	Binding	pKi	=	106.00	6.97	7	4	-	PDSP KiDatabase	961.4	29	13	12	-1.46	CSCCC(N)C(=O)NC(CCC(=O)O)C(=O)NC(Cc1cnc[nH]1)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCC(=O)O	-
afamelanotide	302	None	19	Human	Binding	Ki	=	0.50	9.30	2	8	Binding affinity towards human Melanocortin 1 receptor (hMC1R)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/s0960-894x(03)00552-3
afamelanotide	302	None	19	Human	Binding	IC50	=	0.51	9.29	2	8	Displacement of [125I]NDP-MSH from Melanocortin 1 receptor at 10 uM	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm960840h
afamelanotide	302	None	19	Human	Binding	IC50	=	0.51	9.29	2	8	Inhibitory concentration against human Melanocortin 1 receptor (hMC1R)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm960845e
afamelanotide	302	None	19	Human	Binding	EC50	=	0.02	10.64	2	8	Effective concentration required for the biological activity against human Melanocortin 1 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm0303103
afamelanotide	302	None	19	Human	Binding	Ki	=	1.80	8.74	2	8	Displacement of Eu-NDP-alphaMSH from human MC1 receptor expressed in human HCT116 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm201226w
afamelanotide	302	None	19	Human	Binding	Ki	=	0.05	10.34	2	8	Displacement of [125I]-NAD-alpha-MSH from human recombinant MC1 receptor expressed in BHK570 cells after 90 mins in presence of ovalbumin	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm201489a
afamelanotide	302	None	19	Mouse	Binding	EC50	=	0.04	10.42	-	8	In vitro activation of mouse recombinant Melanocortin-1 receptor.	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm0104872
afamelanotide	302	None	19	Mouse	Binding	EC50	=	0.04	10.42	-	8	Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm020296e
afamelanotide	302	None	19	Mouse	Binding	EC50	=	0.02	10.74	-	8	Effective concentration for mouse Melanocortin-1 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049010r
afamelanotide	302	None	19	Mouse	Binding	IC50	=	0.31	9.51	-	8	Displacement of 125I-NDP-MSH from mouse MC1R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.5b01894
afamelanotide	302	None	19	Mouse	Binding	IC50	=	0.29	9.54	-	8	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 1 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.9b00860
agouti	314	None	0	Mouse	Binding	pKd	None	-	8.60	19	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/7935841
agouti	314	None	0	Mouse	Binding	pKd	None	-	8.60	19	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9454589

Showing 1 to 20 of 1,172 entries

Search:

	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

α-MSH	366	None	0	Human	Functional	pIC50	None	-	8.40	-	4	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12007532
[D-Trp⁸]γ-MSH	1501	None	4	Human	Functional	EC50	=	300.00	6.52	-1	4	Agonist activity at human MC1R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation measured after 3 mins	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.7b01295
[D-Trp⁸]γ-MSH	1501	None	4	Human	Functional	EC50	=	300.00	6.52	-1	4	Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049579s
[D-Trp⁸]γ-MSH	1501	None	4	Human	Functional	EC50	=	70.00	7.16	-1	4	Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049579s
afamelanotide	302	None	19	Human	Functional	pIC50	None	-	10.00	-2	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12007532
afamelanotide	302	None	19	Human	Functional	pIC50	None	-	10.00	-2	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/3286233
afamelanotide	302	None	19	Human	Functional	EC50	=	0.07	10.15	-2	8	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/s0960-894x(03)00552-3
afamelanotide	302	None	19	Human	Functional	EC50	=	0.19	9.72	-2	8	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 1 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm960840h
afamelanotide	302	None	19	Human	Functional	EC50	=	0.19	9.72	-2	8	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm960845e
afamelanotide	302	None	19	Human	Functional	EC50	=	0.50	9.30	-2	8	Agonist activity against human melanocortin receptor hMC1R	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/s0960-894x(02)00830-2
afamelanotide	302	None	19	Human	Functional	EC50	=	0.50	9.30	-2	8	Agonist potency for human Melanocortin 1 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/s0960-894x(02)00459-6
afamelanotide	302	None	19	Human	Functional	EC50	=	0.02	10.64	-2	8	Evaluated for agonist activity at cloned mammalian human MSH1 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm00018a005
afamelanotide	302	None	19	Human	Functional	EC50	=	0.07	10.15	-2	8	Agonist activity at human MC1R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.8b00251
afamelanotide	302	None	19	Mouse	Functional	EC50	=	0.04	10.42	1	8	Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm010524p
afamelanotide	302	None	19	Mouse	Functional	EC50	=	0.05	10.34	1	8	Maximal agonist response of mouse melanocortin 1 receptor (MC1R)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm030452x
afamelanotide	302	None	19	Mouse	Functional	EC50	=	12.00	7.92	1	8	Agonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/s0960-894x(03)00318-4
afamelanotide	302	None	19	Mouse	Functional	EC50	=	0.38	9.42	1	8	Effective concentration against mouse Melanocortin 1 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm0303608
afamelanotide	302	None	19	Mouse	Functional	EC50	=	0.03	10.52	1	8	Functional activity at the mouse melanocortin 1 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm010061n
afamelanotide	302	None	19	Mouse	Functional	EC50	=	0.03	10.49	1	8	In vitro agonist potency for Mouse Melanocortin 1 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm0490843
afamelanotide	302	None	19	Mouse	Functional	EC50	=	0.02	10.64	1	8	Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm0492756

Showing 1 to 20 of 1,251 entries

Join us

Cite us

Main reference

Ligand source activities (1 row/activity)